A series of N-(2,4-difluorophenyl)-N′-heptyl-N′-{4- [(substituted)-pyridazin-3-yl)thio]pentyl}urea derivatives having a phenyl ring at positions 5 and/or at position 6 of the heterocycle, as well as the corresponding sulfones, were synthesized. Their inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT) was tested on the enzyme prepared from rat liver microsomes. Theoretical studies were performed to correlate their activity to their structural features.
Gelain, A., Bettinelli, I., Barlocco, D., Kwon Byoung, M., Jeong Tae, S., Im Kyung, R., et al. (2006). Ureidopyridazine derivatives as acyl-CoA:cholesterol acyltransferase inhibitors. SCIENTIA PHARMACEUTICA, 74(3), 85-97 [10.3797/scipharm.2006.74.85].
Ureidopyridazine derivatives as acyl-CoA:cholesterol acyltransferase inhibitors
LEGNANI, LAURA;
2006
Abstract
A series of N-(2,4-difluorophenyl)-N′-heptyl-N′-{4- [(substituted)-pyridazin-3-yl)thio]pentyl}urea derivatives having a phenyl ring at positions 5 and/or at position 6 of the heterocycle, as well as the corresponding sulfones, were synthesized. Their inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT) was tested on the enzyme prepared from rat liver microsomes. Theoretical studies were performed to correlate their activity to their structural features.
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